Synthesis and biological evaluation of novel N-methyl-picolinamide-4-thiol derivatives as potential antitumor agents.

A novel series of N-methylpicolinamide-4-thiol derivatives were synthesized and evaluated on human cancer cell lines. Among them, compound 6p displayed potent and broad-spectrum anti-proliferative activities in vitro on some human cancer cell lines, even better than sorafenib. The advanced kinase inhibitory assays showed that compound 6p could selectively inhibit Aurora-B kinase.

6-Chloro-3-nitro-N-(propan-2-yl)pyridin-2-amine.

There are two mol-ecules in the asymmetric unit mol-ecule of the title compound, C(8)H(10)ClN(3)O(2). Intra-molecular N-H⋯O hydrogen bonds stabilize the mol-ecular structure. There are no classical inter-molecular hydrogen bonds in the crystal structure.

(2-Chloro-3,5-dinitro-phen-yl)(piperidin-1-yl)methanone.

In the title compound, C(12)H(12)ClN(3)O(5), the piperidine ring adopts a chair conformation. One of the nitro groups is almost coplanar with the aromatic ring [O-N-C-C = -1.4 (2)°], whereas the other one is significantly twisted out of the ring plane [O-N-C-C = 34.